1. GPCR/G Protein
    MAPK/ERK Pathway
  2. Ras
    p38 MAPK
  3. BI-3406

BI-3406 

Cat. No.: HY-125817 Purity: 99.51% ee.: 98.04%
Handling Instructions

BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity.

For research use only. We do not sell to patients.

BI-3406 Chemical Structure

BI-3406 Chemical Structure

CAS No. : 2230836-55-0

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 356 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2000 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity[1][2].

IC50 & Target[1]

KRAS-SOS1

6 nM (IC50)

In Vitro

BI-3406 is an inhibitor of the interaction between KRAS and its Guanine Nucleotide Exchange Factor (GEF) SOS1. BI-3406 does not block the interaction of KRAS with SOS2 but elicits activity on a broad panel of KRAS oncogenic variants, including all major G12 and G13 oncoproteins. Down-modulation of this signaling cascade by BI-3406 in KRAS G12 or G13 mutant cells effectively limits cell proliferation[2].

Molecular Weight

462.46

Formula

C₂₃H₂₅F₃N₄O₃

CAS No.

2230836-55-0

SMILES

CC1=NC(N[[email protected]@H](C2=CC(C(F)(F)F)=CC(N)=C2)C)=C3C=C(O[[email protected]@H]4COCC4)C(OC)=CC3=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (216.23 mM; Need ultrasonic)

Ethanol : 100 mg/mL (216.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1623 mL 10.8117 mL 21.6235 mL
5 mM 0.4325 mL 2.1623 mL 4.3247 mL
10 mM 0.2162 mL 1.0812 mL 2.1623 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.41 mM); Clear solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

  • 5.

    Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

  • 6.

    Add each solvent one by one:  10% EtOH    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.51% ee.: 98.04%

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Keywords:

BI-3406BI3406BI 3406Rasp38 MAPKorallyinteractionKRASSonofSevenless1SOS1GTP-loadedanticancerInhibitorinhibitorinhibit

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Product name:
BI-3406
Cat. No.:
HY-125817
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